Structure‐based design, synthesis, and evaluation of Bcl‐2/Mcl‐1 dual inhibitors

Design, synthesis and preliminary bioactivity studies of indomethacin derivatives as Bcl-2/Mcl-1 dual inhibitors

(2019) Chen Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery and development of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as Bcl-2/Mcl-1 inhibitors

(2019) Renshuai Liu et al.   BIOORGANIC CHEMISTRY

Hot-Spots of Mcl-1 Protein

(2019) Camille Denis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Using CETSA assay and a mathematical model to reveal dual Bcl-2/Mcl-1 inhibition and on-target mechanism for ABT-199 and S1

(2019) Zongwei Guo et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A

(2018) Alma Abou Samra et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

BCL-2 selective inhibitor ABT-199 primes rhabdomyosarcoma cells to histone deacetylase inhibitor-induced apoptosis

(2018) Ulrike Heinicke et al.   ONCOGENE

Combining BH3-mimetics to target both BCL-2 and MCL1 has potent activity in pre-clinical models of acute myeloid leukemia

(2018) Donia M. Moujalled et al.   LEUKEMIA

BIS overexpression does not affect the sensitivity of HEK 293T cells against apoptosis

(2017) Ji-Ye Baek et al.   Molecular & Cellular Toxicology

From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors

(2017) Avi Ashkenazi et al.   NATURE REVIEWS DRUG DISCOVERY

Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules

(2016) Jeremy L. Yap et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Mcl-1/Bcl-2 Dual Inhibitors Created by the Structure-Based Hybridization of Drug-Divided Building Blocks and a Fragment Deconstructed from a Known Two-Face BH3 Mimetic

(2015) Zhichao Zhang et al.   ARCHIV DER PHARMAZIE

Emerging understanding of Bcl-2 biology: Implications for neoplastic progression and treatment

(2015) Cristina Correia et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

ABT-199 (venetoclax) and BCL-2 inhibitors in clinical development

(2015) Shundong Cang et al.   Journal of Hematology & Oncology

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

(2013) Andrew J Souers et al.   NATURE MEDICINE

Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy

(2013) Peter E. Czabotar et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1

(2012) Ting Song et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Deciphering the rules of programmed cell death to improve therapy of cancer and other diseases

(2011) Andreas Strasser et al.   EMBO JOURNAL

Probing the difference between BH3 groove of Mcl-1 and Bcl-2 protein: Implications for dual inhibitors design

(2011) Zhichao Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

SAR by Interligand Nuclear Overhauser Effects (ILOEs) Based Discovery of Acylsulfonamide Compounds Active against Bcl-xLand Mcl-1

(2011) Michele F. Rega et al.   JOURNAL OF MEDICINAL CHEMISTRY

3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) Based Molecules as Potent, Dual Inhibitors of B-Cell Lymphoma 2 (Bcl-2) and Myeloid Cell Leukemia Sequence 1 (Mcl-1): Structure-Based Design and Structure−Activity Relationship Studies

(2011) Zhichao Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mcl-1; the molecular regulation of protein function

(2010) Luke W. Thomas et al.   FEBS LETTERS

A novel BH3 mimetic S1 potently induces Bax/Bak-dependent apoptosis by targeting both Bcl-2 and Mcl-1

(2010) Zhichao Zhang et al.   INTERNATIONAL JOURNAL OF CANCER

Therapeutic targeting of apoptosis pathways in cancer

(2009) David S Ziegler et al.   CURRENT OPINION IN ONCOLOGY

Bcl-xLand MCL-1 constitute pertinent targets in ovarian carcinoma and their concomitant inhibition is sufficient to induce apoptosis

(2009) Emilie Brotin et al.   INTERNATIONAL JOURNAL OF CANCER